A GRP/bombesin receptor 2 antagonist (IC50 = 4.13 nM in vitro); reduces bombesin-stimulated pancreatic amylase secretion and attenuates bombesin-stimulated increases in blood pressure in rats

ICI 216140 – 500 µg

Brand:
Cayman
CAS:
124001-41-8
Storage:
-20
UN-No:
Non-Hazardous - /

Bombesin is a peptide, originally isolated from the skin of the European fire-bellied toad, with pressor and sympathoexcitatory activity. Its three receptors are distributed throughout the central and peripheral nervous system and are involved in gastric acid secretion, emotional response, temperature control, learning, and memory. Neuromedin B and gastrin-releasing peptide (GRP) are mammalian homologs of bombesin.{28635} ICI 216140 is a GRP/bombesin receptor 2 antagonist (IC50 = 2 nM in vitro).{28634} At 2 mg/kg, it can reduce bombesin-stimulated pancreatic amylase secretion in rats.{28634} At 1 mM, it has been shown to attenuate bombesin-stimulated increases in blood pressure in rats.{28636}  

 

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Description

A GRP/bombesin receptor 2 antagonist (IC50 = 4.13 nM in vitro); reduces bombesin-stimulated pancreatic amylase secretion and attenuates bombesin-stimulated increases in blood pressure in rats

Formal name: N-(2-methyl-1-oxopropyl)-7-D-alanine-9-(N-methyl-L-leucinamide)-3-9-neuromedin C

Synonyms: 

Molecular weight: 916.1

CAS: 124001-41-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Endocrinology & Metabolism

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